Avandamet

Generic Name: osiglitazone maleate and metformin hydrochloride
Brand Name: Avandamet

Indications

Avandamet is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Regular exercise and proper diet should be maintained while taking this medication.

Dosage and Administration

Avandamet tablet contains rosiglitazone as the maleate and metformin hydrochloride and is available as 2 mg/500 mg, 4 mg/500 mg, 2 mg/1,000 mg and 4 mg/1,000 mg tablets.

Normal dosage: recommended dosage is on the basis of effectiveness and tolerability while not exceeding the maximum recommended daily dose of 8 mg/2,000 mg. Avandamet is generally given in divided doses with meals, with gradual dose escalation. This reduces gastrointestinal side effects (largely due to metformin) and permits determination of the minimum effective dose for the individual patient.

Overdosage: An overdose is likely to cause lactic acidosis. Symptoms of lactic acidosis include a feeling of general discomfort or sickness; weakness; sore or aching muscles; trouble breathing; unusual drowsiness, dizziness or lightheadedness and the sudden development of a slow or irregular heartbeat.

 

Drug Description

Rosiglitazone maleate is an oral antidiabetic agent, which acts primarily by increasing insulin sensitivity. Rosiglitazone improves glycemic control while reducing circulating insulin levels. Pharmacologic studies in animal models indicate that rosiglitazone improves sensitivity to insulin in muscle and adipose tissue and inhibits hepatic gluconeogenesis. Rosiglitazone maleate is not chemically or functionally related to the sulfonylureas, the biguanides, or the α-glucosidase inhibitors.

Chemically, rosiglitazone maleate is (±)-5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl] methyl]-2,4-thiazolidinedione, (Z)-2-butenedioate (1:1) with a molecular weight of 473.52 (357.44 free base). The molecule has a single chiral center and is present as a racemate. Due to rapid interconversion, the enantiomers are functionally indistinguishable. The molecular formula is C18H19N3O3S•C4H4O4. Rosiglitazone maleate is a white to off-white solid with a melting point range of 122°to 123°C. The pKa values of rosiglitazone maleate are 6.8 and 6.1. It is readily soluble in ethanol and a buffered aqueous solution with pH of 2.3; solubility decreases with increasing pH in the physiological range. The structural formula of rosiglitazone maleate is:

Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is not chemically or pharmacologically related to any other classes of oral antihyperglycemic agents. Metformin hydrochloride is a white to off-white crystalline compound with a molecular formula of C4H11N5•HCl and a molecular weight of 165.63. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride is 6.68.
The structural formula of metformin hydrochloride is:

Side Effects

The common side effects noted are Nausea, Diarrhea, headache, dyspepsia, dizziness, edema, abdominal pain, constipation, influenza and so on

Precautions

• Avoid alcohol intake while taking Avandamet.
• This medication should be avoided during pregnancy.
• Metformin and rosiglitazone does not usually cause hypoglycemia (low blood sugar). Hypoglycemia may occur, as a result of skipped meals, excessive exercise, or alcohol consumption. Know the signs and symptoms of low blood sugar, which include hunger, headache, drowsiness, weakness, dizziness, a fast heartbeat, perspiration, tremor, and nausea.

Drug Interactions

Avoid the following:

• Rosiglitazone potentiated by CYP2C8 inhibitors (eg, gemfibrozil).
• Metforming potentiated by cationic drugs eliminated by renal tubular secretion (eg, amiloride, cimetidine, digoxin, procainamide, quinidine and ranitidine).
• Hyperglycemia with diuretics, steroids, phenytoin, phenothiazines, nicotinic acid, isoniazid.

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